[CAS NO. 167933-07-5] Flibanserin

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PRODUCTS SPECIFICATIONS [167933-07-5]

Catalog

AS425091

Brand

Arctom Scientific

CAS

167933-07-5

DESCRIPTION [167933-07-5]

Overview

MDL	MFCD00918402
Molecular Weight	390.40
Molecular Formula	C20H21F3N4O
SMILES	O=C1NC2=CC=CC=C2N1CCN3CCN(C4=CC=CC(C(F)(F)F)=C4)CC3

For research use only. We do not sell to patients.

Summary

Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with K _i values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an K _i value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research ^[1] ^- ^[5] .

IC50 & Target

5-HT _1A Receptor

1 nM (Ki)

5-HT _2A Receptor

49 nM (Ki)

dopamine D4 receptors

4-24 nM (Ki)

In Vitro

Flibanserin (0.01-100 μM; 72 h) can transform into two degradation products DP1 and DP2 with no toxicity potential after oxidative degradation ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[1]

Cell Line:	NHSF cell lin
Concentration:	0.01, 0.1, 1, 10, 100 μM
Incubation Time:	72 hours
Result:	Resulted cell viability reached to 97.91% (DP1) and 96.73% (DP2) at 0.01 μM. Showed non-toxic up to 100 μM (IC ₅₀ >100 μM).

In Vivo

Flibanserin (1, 10, 30 mg/kg; i.p.; single dose) shows different pharmacological properties in prefrontal cortex, hippocampus and midbrain. The 5-HT1A receptor occupancy in cortex indicates it’s the more sensitive than other brain region ^[2] .
Flibanserin (15, 45 mg/kg; p.o.; twice a day; 22 d) preferentially activates the brain regions belonging to the mesolimbic dopaminergic pathway and hypothalamic structures involved in the integration of sexual cues related to sexual motivation ^[3] .
Flibanserin (5, 10, 25, and 50 mg/kg; s.c.; single dose) has anxiolytic effects without locomotor side effects in rat ultrasonic vocalization model ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Long Evans female rats (225-250 g) ^[3]
Dosage:	15 mg/kg; 45 mg/kg
Administration:	Oral gavage; twice a day for 22 days
Result:	Increased the density of activated catecholaminergic neurons in the ventral tegmental area but not in the locus coeruleus. Increased Fos expression in the medial preoptic area and arcuate nucleus of the hypothalamus, ventral tegmental area, locus coeruleus, and lateral paragigantocellular nucleus with chronic 22-day treatment.

Animal Model:	Rat pup ultrasonic vocalization model of anxiety ^[4]
Dosage:	5, 10, 25, and 50 mg/kg
Administration:	Subcutaneous injection
Result:	Reduced ultrasonic vocalizations in rat pups. Showed effective within 30 min and has no severe locomotor side effects at active doses.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04002661	Mohit Khera\|Sprout Pharmaceuticals, Inc\|Baylor College of Medicine	Low Libido	May 8, 2020	Phase 2
NCT00601367	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	January 2008	Phase 3
NCT00441558	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	February 2007	Phase 3
NCT01188603	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	July 2010	Phase 1
NCT01057901	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	January 2010	Phase 3
NCT00360529	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	July 2006	Phase 3
NCT01103362	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	April 2010	Phase 3
NCT01040208	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological\|Depression	January 2010	Phase 3
NCT00360555	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	July 2006	Phase 3
NCT01134965	Boehringer Ingelheim	Healthy	June 2010	Phase 1
NCT00277914	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	January 2006	Phase 3
NCT03707340	Memorial Sloan Kettering Cancer Center	Breast Cancer\|Hyposexual Desire Disorder	September 14, 2018
NCT04743934	Andrew McDonald\|University of Alabama at Birmingham	Prostate Adenocarcinoma	July 2, 2021	Phase 2
NCT04494191	Genuine Research Center, Egypt\|Bio Med for Pharmaceuticals Industries (BIOMED), Egypt	Healthy	December 12, 2018	Phase 1
NCT00360243	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	July 2006	Phase 3
NCT00996164	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	October 2009	Phase 3
NCT02714049	San Diego Sexual Medicine	Hypoactive Sexual Desire Disorder	January 25, 2017	Phase 4
NCT00996372	Sprout Pharmaceuticals, Inc	Sexual Dysfunctions, Psychological	October 2009	Phase 3
NCT02770768	University of Chicago	Hypoactive Sexual Desire Disorder	October 2016	Not Applicable

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 128.07 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5615 mL	12.8074 mL	25.6148 mL
5 mM	0.5123 mL	2.5615 mL	5.1230 mL
10 mM	0.2561 mL	1.2807 mL	2.5615 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

2H-Benzimidazol-2-one, 1,3-dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-

1,3-Dihydro-1-[2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl]-2H-benzimidazol-2-one

BIMT 17

Flibanserin

BIMT 17BS

Addyi

1-(2-[4-[3-(Trifluoromethyl)phenyl]piperazin-1-yl]ethyl)-1,3-dihydro-2H-benzimidazol-2-one